Description:
Mode of action:
Diclofenac sodium, a non-steroidal anti-inflammatory compound exhibits pronounced antirheumatic, anti-inflammatory, analgesic, and antipyretic properties. Its mode of action is not known; however, its ability to inhibit prostaglandin synthesis may be involved in the anti-inflammatory effect.
Pharmacokinetics:
Enteric coated Tablets: Diclofenac is completely absorbed from the enteric coated tablets after their passage through the stomach; the mean peak plasma concentration is attained on average 2 hours after ingestion of one tablet of 50 mg.
Suppositories: Diclofenac shows a rapid onset of absorption from suppositories, after the administration of 50 mg suppositories, peak plasma concentrations are attained on average within 1 hour
Extended release tablet: After ingestion of the diclofenac slow release tablet, it is slowly released into the gastrointestinal contents, Peak plasma concentrations occur about 6-8 hours after administration of the XR tablets when taken with a meal.
Following oral or rectal administration, the active substance is metabolised during its first passage through the liver, Diclofenac bounds to serum proteins 99.7%, mainly to albumin. About 60% of the administered dose is excreted in urine as metabolites. Less than 1% is excreted as unchanged substance. The rest is eliminated as metabolites through the bile in the faeces.
Indications:
Enteric coated tablets:
- Inflammatory and degenerative forms of rheumatism: rheumatoid arthritis and osteoarthritis.
- Relief of acute or chronic pain states in which there is an inflammatory component.
- Symptomatic treatment of primary dysmenorrhoea.
Suppositories:
- Inflammatory and degenerative forms of rheumatism: rheumatoid arthritis and osteoarthritis.
- Short term (up to three days) treatment of post-operative pain in children
XR Tablets:
- For both (100 mg, 75 mg): in the management of chronic conditions, such as rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis
- For 75 mg: acute gout, acute musculoskeletal disorders such as periarthritis (for example frozen shoulder), tendinitis, tenosynovitis, bursitis, other painful conditions resulting from trauma, including fracture, low back pain, sprains, strains, dislocations, orthopaedic, dental and other minor surgery.
Contraindications:
- hypersensitivity to the active ingredient or any of the excipients
- Gastric, intestinal (e.g. duodenal) ulcer, gastro-intestinal bleeding or perforation.
- History of gastrointestinal bleeding or perforation, relating to previous NSAID therapy. Active, or history of recurrent peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding)
- Last trimester of pregnancy
- Severe hepatic (impairment), renal or cardiac failure.
- Established congestive heart failure (NYHA IIIV), ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease.
- Treatment of perioperative pain in setting of coronary artery bypass graft surgery (CABG)
- Patients in whom diclofenac, aspirin or other NSAIDs induce asthma, urticaria or other allergic-type reactions, because severe, rarely fatal, anaphylactic type reactions to diclofenac have been reported in such patients.
- Proctitis (only for suppositories)